Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression

Cyclic GMP-AMP synthase (cGAS) is involved in the modulation of inflammatory responses. Here, the authors present small-molecule inhibitors of human cGAS, characterize their interaction with the protein, and show that the compounds are active in interferon-producing cells including primary human mac...

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Autores principales: Lodoe Lama, Carolina Adura, Wei Xie, Daisuke Tomita, Taku Kamei, Vitaly Kuryavyi, Tasos Gogakos, Joshua I. Steinberg, Michael Miller, Lavoisier Ramos-Espiritu, Yasutomi Asano, Shogo Hashizume, Jumpei Aida, Toshihiro Imaeda, Rei Okamoto, Andy J. Jennings, Mayako Michino, Takanobu Kuroita, Andrew Stamford, Pu Gao, Peter Meinke, J. Fraser Glickman, Dinshaw J. Patel, Thomas Tuschl
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Lenguaje:EN
Publicado: Nature Portfolio 2019
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Acceso en línea:https://doaj.org/article/6f06ae155ca2436dab39b0d693daf384
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spelling oai:doaj.org-article:6f06ae155ca2436dab39b0d693daf3842021-12-02T16:57:44ZDevelopment of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression10.1038/s41467-019-08620-42041-1723https://doaj.org/article/6f06ae155ca2436dab39b0d693daf3842019-05-01T00:00:00Zhttps://doi.org/10.1038/s41467-019-08620-4https://doaj.org/toc/2041-1723Cyclic GMP-AMP synthase (cGAS) is involved in the modulation of inflammatory responses. Here, the authors present small-molecule inhibitors of human cGAS, characterize their interaction with the protein, and show that the compounds are active in interferon-producing cells including primary human macrophages.Lodoe LamaCarolina AduraWei XieDaisuke TomitaTaku KameiVitaly KuryavyiTasos GogakosJoshua I. SteinbergMichael MillerLavoisier Ramos-EspirituYasutomi AsanoShogo HashizumeJumpei AidaToshihiro ImaedaRei OkamotoAndy J. JenningsMayako MichinoTakanobu KuroitaAndrew StamfordPu GaoPeter MeinkeJ. Fraser GlickmanDinshaw J. PatelThomas TuschlNature PortfolioarticleScienceQENNature Communications, Vol 10, Iss 1, Pp 1-14 (2019)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
Lodoe Lama
Carolina Adura
Wei Xie
Daisuke Tomita
Taku Kamei
Vitaly Kuryavyi
Tasos Gogakos
Joshua I. Steinberg
Michael Miller
Lavoisier Ramos-Espiritu
Yasutomi Asano
Shogo Hashizume
Jumpei Aida
Toshihiro Imaeda
Rei Okamoto
Andy J. Jennings
Mayako Michino
Takanobu Kuroita
Andrew Stamford
Pu Gao
Peter Meinke
J. Fraser Glickman
Dinshaw J. Patel
Thomas Tuschl
Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression
description Cyclic GMP-AMP synthase (cGAS) is involved in the modulation of inflammatory responses. Here, the authors present small-molecule inhibitors of human cGAS, characterize their interaction with the protein, and show that the compounds are active in interferon-producing cells including primary human macrophages.
format article
author Lodoe Lama
Carolina Adura
Wei Xie
Daisuke Tomita
Taku Kamei
Vitaly Kuryavyi
Tasos Gogakos
Joshua I. Steinberg
Michael Miller
Lavoisier Ramos-Espiritu
Yasutomi Asano
Shogo Hashizume
Jumpei Aida
Toshihiro Imaeda
Rei Okamoto
Andy J. Jennings
Mayako Michino
Takanobu Kuroita
Andrew Stamford
Pu Gao
Peter Meinke
J. Fraser Glickman
Dinshaw J. Patel
Thomas Tuschl
author_facet Lodoe Lama
Carolina Adura
Wei Xie
Daisuke Tomita
Taku Kamei
Vitaly Kuryavyi
Tasos Gogakos
Joshua I. Steinberg
Michael Miller
Lavoisier Ramos-Espiritu
Yasutomi Asano
Shogo Hashizume
Jumpei Aida
Toshihiro Imaeda
Rei Okamoto
Andy J. Jennings
Mayako Michino
Takanobu Kuroita
Andrew Stamford
Pu Gao
Peter Meinke
J. Fraser Glickman
Dinshaw J. Patel
Thomas Tuschl
author_sort Lodoe Lama
title Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression
title_short Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression
title_full Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression
title_fullStr Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression
title_full_unstemmed Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression
title_sort development of human cgas-specific small-molecule inhibitors for repression of dsdna-triggered interferon expression
publisher Nature Portfolio
publishDate 2019
url https://doaj.org/article/6f06ae155ca2436dab39b0d693daf384
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